The compound of Formula I is cyclic polypeptide compound, i.e., Micafungin. Following Caspofungin, Micafungin Sodium (FK463, Tradename: Mycamine; Fujisawa Co.) is the second echinocandin antifungal medicament approved by FDA, the structure of which is shown in Formula III. Micafungin is obtained by chemically modifying the fermentation product of Coleophoma empedrit. Micafungin was firstly marketed in Japan in 2002, and approved by FDA and marketed in US in May 2005. Clinical test has demonstrated that Micafungin is very efficient for treating Candida and Aspergillus, and can be used as first-line medicine for treating diseases caused by Candida infections.
Since Micafungin and the salts thereof are generally unstable to light, heat, humidity, acid, and the like, it is urgent to develop a pharmaceutical composition for stabilizing the compound and the salts thereof. CN 1179748C has disclosed a stable pharmaceutical composition of Micafungin in lyophilized form comprising lactose as stabilizing agent. CN 100352495C has disclosed a stable pharmaceutical composition of Micafungin in lyophilized form comprising maltose as stabilizing agent. However, both of the pharmaceutical compositions are not ideal in stability. The inventors have unexpectedly discovered that compared with both of the above compositions, the pharmaceutical composition of compound of Formula I comprising trehalose as stabilizing agent is by far stable.
The composition provided by the present invention is a safe, stable and reproducible lyophilized formulation, and can be directly used to treat/prevent infectious diseases.